GADOTERATE MEGLUMINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GADOTERATE MEGLUMINE (GADOTERATE MEGLUMINE).
Gadoterate meglumine is a paramagnetic contrast agent that increases the relaxation rate of water protons in tissues, thereby enhancing image contrast in magnetic resonance imaging (MRI). It is a macrocyclic gadolinium-based contrast agent (GBCA) with high thermodynamic stability and kinetic inertness, reducing the risk of gadolinium dissociation.
| Metabolism | Gadoterate meglumine is not metabolized. It is eliminated unchanged predominantly via renal glomerular filtration. |
| Excretion | Primarily renal (99% excreted unchanged in urine within 24 hours); biliary/fecal elimination negligible (<1%). |
| Half-life | Terminal elimination half-life approximately 1.5–2 hours in patients with normal renal function; prolonged in renal impairment (up to 12–34 hours in severe impairment). |
| Protein binding | Minimal protein binding (<1%). |
| Volume of Distribution | Approximately 0.2 L/kg, suggesting distribution primarily within extracellular fluid. |
| Bioavailability | Not applicable; administered intravenously only (100% bioavailability by IV route). |
| Onset of Action | Immediate upon intravenous injection (MRI enhancement observed within minutes); no other routes of clinical relevance. |
| Duration of Action | Enhancement persists for 1–2 hours post-injection; imaging window typically 30–60 minutes; may be longer in patients with renal impairment. |
0.2 mL/kg (0.1 mmol/kg) intravenously as a single bolus injection.
| Dosage form | SOLUTION |
| Renal impairment | GFR 30-60 mL/min/1.73m2: No dose adjustment necessary. GFR <30 mL/min/1.73m2: Not recommended; use alternative agent if possible. In patients on dialysis, only administer if diagnostic information is essential; no supplemental dose after dialysis. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment. For severe hepatic impairment (Child-Pugh C): Use caution, consider benefit-risk, as elimination may be prolonged. |
| Pediatric use | Neonates (≥1 week) to adults: 0.2 mL/kg (0.1 mmol/kg) intravenously. For children <1 week: 0.2 mL/kg (0.1 mmol/kg) intravenously. |
| Geriatric use | No specific dose adjustment required based on age alone. Assess renal function before administration; consider lower dose if GFR <30 mL/min/1.73m2. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GADOTERATE MEGLUMINE (GADOTERATE MEGLUMINE).
| Breastfeeding | Gadoterate meglumine is excreted into breast milk in small amounts. The milk-to-plasma (M/P) ratio was 0.014 in a single study; absolute infant dose is <0.04% of maternal weight-adjusted dose. The American College of Radiology recommends that breastfeeding may be continued without interruption after gadoterate administration, but informed discussion with the mother is advised. If concern persists, the mother may pump and discard milk for 24 hours. |
| Teratogenic Risk | Gadoterate meglumine is a gadolinium-based contrast agent (GBCA). In the first trimester, gadolinium crosses the placenta and has been associated with a potential but unconfirmed risk of congenital anomalies based on animal studies; human data are limited. In the second and third trimesters, gadolinium exposure increases the risk of stillbirth, neonatal death, and rheumatic/inflammatory skin conditions in the offspring. GBCAs accumulate in fetal membranes and breast milk; clinical use is contraindicated unless essential and only at the lowest possible dose. |
■ FDA Black Box Warning
Gadolinium-based contrast agents (GBCAs) increase the risk for nephrogenic systemic fibrosis (NSF) in patients with chronic, severe kidney disease (glomerular filtration rate [GFR] < 30 mL/min/1.73 m²) or acute kidney injury. Patients with these conditions should avoid use of GBCAs unless the diagnostic information is essential and not available with non-contrast MRI.
| Serious Effects |
["History of hypersensitivity (anaphylaxis or severe allergic reaction) to gadoterate meglumine or any component of the formulation","Chronic severe kidney disease (GFR < 30 mL/min/1.73 m²) or acute kidney injury, unless the diagnostic information is essential and not available with non-contrast MRI"]
| Precautions | ["Nephrogenic systemic fibrosis (NSF): Risk increased in patients with chronic severe kidney disease (GFR < 30 mL/min/1.73 m²) or acute kidney injury; screen all patients for renal impairment before use.","Acute adverse reactions: Serious anaphylactoid reactions, including death, have occurred; emergency equipment and trained personnel should be available.","Gadolinium retention: Gadolinium is retained for months to years in brain, bone, skin, and other organs; implications are not fully understood but may be relevant for patients undergoing multiple lifetime doses.","Impaired renal function: In patients with moderately impaired renal function (GFR 30-60 mL/min/1.73 m²), use the lowest possible dose and monitor for signs of NSF.","Pregnancy: Use only if clearly needed; gadolinium crosses the placenta and may be retained in fetal tissues."] |
Loading safety data…
| Fetal Monitoring | Monitor maternal renal function prior to administration as gadoterate is eliminated renally. In severe renal impairment, risks of nephrogenic systemic fibrosis (NSF) must be weighed. During pregnancy, fetal heart rate monitoring is not specifically required for contrast administration, but standard obstetric monitoring during any medical procedure applies. Gadoterate is contraindicated in pregnancy unless essential; if used, limit to lowest dose and document the need. |
| Fertility Effects | No human data; animal studies (rat) showed no adverse effects on fertility, reproductive performance, or early embryonic development at clinically relevant doses. Sperm abnormalities were not reported. No clinically significant impact on fertility is expected. |